HOT: Synthesis and biological evaluation of 4,5-disubstituted isoquinolin-1-ones

Michael D. Threadgill and coworkers at University of Bath report a very interesting synthesis of 4,5-disubstituted isoquinolin-1-ones and their biological evaluation against PARP-2.

This paper is specially relevant because of the difficulties of working with this class of compound such as insolubility and lack of reactivity. This is a HOT paper that will be free to access until 6th December.

A very neat synthesis relevant for the synthetic and medicinal chemistry communities.

Synthesis of 4-alkyl-, 4-aryl- and 4-arylamino-5-aminoisoquinolin-1-ones and identification of a new PARP-2 selective inhibitor
Peter T. Sunderland, Archana Dhami, Mary F. Mahon, Louise A. Jones, Sophie R. Tully, Matthew D. Lloyd, Andrew S. Thompson, Hashim Javaid, Niall M. B. Martin and Michael D. Threadgill
Org. Biomol. Chem., 2011, Advance Article
DOI: 10.1039/C0OB00665C,

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